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transporter activator

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

6

Natural
Products

2

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-139692
    EAAT2 activator 1

    		EAAT Neurological Disease
    EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently .
    EAAT2 activator 1
  • HY-111928
    5,7-Dimethoxyluteolin

    		Dopamine Transporter Neurological Disease
    5,7-Dimethoxyluteolin, a 5,7-dimethylluteolin derivative, is a dopamine transporter (DAT) activator with an EC50 of 3.417 μM .
    5,7-Dimethoxyluteolin
  • HY-12741
    LDN-212320
    Maximum Cited Publications
    9 Publications Verification

    LDN-0212320; OSU-0212320

    		 EAAT Neurological Disease
    LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC [1]
    LDN-212320
  • HY-161724
    TFEB activator 2

    		Amyloid-β Dopamine Transporter CDK Autophagy Neurological Disease
    TFEB activator 2 is an orally active compound that can cross the blood-brain barrier. TFEB activator 2 can bind to the dopamine transporter (DAT). TFEB activator 2 promotes TFEB nuclear translocation and lysosome biogenesis by targeting the DAT-CDK9-TFEB pathway. TFEB activator 2 has neuroprotective activity and can be used in the research of Alzheimer's disease and other diseases .
    TFEB activator 2
  • HY-B0168A
    Milnacipran hydrochloride
    2 Publications Verification

    		 Serotonin Transporter PERK Neurological Disease
    Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran hydrochloride
  • HY-120950
    S-tram,tram-Farnesylated cysteine methyl ester

    		Amino Acid Derivatives Others
    S-tram,tram-Farnesylated cysteine methyl ester is a multidrug resistance transporter activator. S-tram,tram-Farnesylated cysteine methyl ester acts by stimulating the multidrug resistance transporter ATPase activity and competing for drug binding .
    S-tram,tram-Farnesylated cysteine methyl ester
  • HY-133177
    MS-153

    		EAAT Neurological Disease
    MS-153 is a glutamate transporter activator that can be used as a neuroprotective agent .
    MS-153
  • HY-174145
    GLUT4 activator 3

    		GLUT Metabolic Disease
    GLUT4 activator 3 (Compound 13a) is an antidiabetic agent targeting GLUT4 translocation in skeletal muscle. GLUT4 activator 3 can promote the translocation of glucose transporter 4 (GLUT4) in skeletal muscle cells. GLUT4 activator 3 reduces blood glucose in STZ-induced diabetic rats .
    GLUT4 activator 3
  • HY-B0168
    Milnacipran

    		Serotonin Transporter PERK Neurological Disease
    Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran
  • HY-128038
    N-Desmethyl-loperamide

    		Opioid Receptor Neurological Disease
    N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
    N-Desmethyl-loperamide
  • HY-B0168S
    Milnacipran-d10 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran-d10 hydrochloride
  • HY-B0168AS
    Milnacipran-d5 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran-d5 hydrochloride
  • HY-175296
    EAAT2 activator 2

    		EAAT Neurological Disease
    EAAT2 activator 2 (Compound 4(SF-2)) is a brain-penetrant excitatory amino acid transporter 2 (EAAT2) modulator (Ki=28.7 nM). EAAT2 activator 2 enhances EAAT2-mediated glutamate uptake, improving synaptic glutamate clearance. EAAT2 activator 2 is promising for research of neurodegenerative diseases (e.g., ALS, Alzheimer’s disease) .
    EAAT2 activator 2
  • HY-B0168AR
    Milnacipran hydrochloride (Standard)

    		Reference Standards Serotonin Transporter PERK Neurological Disease
    Milnacipran (hydrochloride) (Standard) is the analytical standard of Milnacipran hydrochloride (HY-B0168A). This product is intended for research and analytical applications. Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
    Milnacipran hydrochloride (Standard)
  • HY-116003
    12,13-DiHOME

    		Endogenous Metabolite Metabolic Disease
    12,13-DiHOME is a stimulator of Brown adipose tissue (BAT), as well as a thermogenic lipokine that activates BAT in response to cold. (±)12,13-DiHOME activates BAT fuel uptake and enhances cold tolerance, via promoting the translocation of the FA transporters FATP1 and CD36 to the cell membrane. (±)12,13-DiHOME can be used for research of metabolic disorders .
    12,13-DiHOME
  • HY-N3504
    Ophiopogonin D'

    		Sirtuin OAT Cancer
    Ophiopogonin D' is a steroidal saponin and a SIRT1 activator. Ophiopogonin D' can also regulate the activities of transporters OATP1B1 and OATP1B3. Ophiopogonin D' exhibits certain toxicity to tumor cells. Ophiopogonin D' can be used in tumor research .
    Ophiopogonin D'
  • HY-161062
    TAOA AM Ester trimethyl lock

    		EAAT Neurological Disease
    TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
    TAOA AM Ester trimethyl lock
  • HY-P10421
    PKCδ substrate

    		ERK Cancer
    PKCδ substrate acts as a nuclear transporter of ERK2 and is involved in ERK2 mediated gene activation. PKCδ is involved in the regulation of cell growth, proliferation, cell cycle arrest, and apoptosis by phosphorylating hBVR and other proteins. PKCδ substrate can be used to study the development of diseases, especially cancer biology .
    PKCδ substrate
  • HY-Y1191
    EEDQ

    EEDQ

    		 Biochemical Assay Reagents 5-HT Receptor Dopamine Transporter Neurological Disease
    EEDQ is a carboxylate activator and irreversible antagonist of 5HT2c receptors. EEDQ reduces [ 3H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates (IC50 = 78.3 μM). EEDQ inhibits contralateral rotation behavior .
    EEDQ
  • HY-174547
    Human PDX1 mRNA

    		mRNA Metabolic Disease
    Human PDX1 mRNA encodes the human pancreatic and duodenal homeobox 1 (PDX1) protein, a transcriptional activator of several genes, including insulin, somatostatin, glucokinase, islet amyloid polypeptide, and glucose transporter type 2. PDX1 may be involved in the early development of the pancreas. It also plays a major role in glucose-dependent regulation of insulin gene expression.
    Human PDX1 mRNA
  • HY-176557
    NCI677397

    		Deubiquitinase Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase Autophagy Cancer
    NCI677397 is a USP24 inhibitor. NCI677397 increases lipid ROS, activates cholesterol and fatty acid biosynthesis, degrades ABC transporters, GPX4 and DHFR through the autophagy pathway, decreases the level of P-gp and ultimately leads to ferroptosis in drug-resistant cancer cells. NCI677397 can be used for the study of lung caner and brain cancer .
    NCI677397
  • HY-W004500
    All-trans-retinal
    1 Publications Verification

    		 Endogenous Metabolite Apoptosis Metabolic Disease
    All-trans-retinal is an vitamin A metabolite in the retina, and is produced following photo-isomerization of the visual chromophore 11-cis-Retinal. All-trans-retinal is cleared from photoreceptors by ATP-binding cassette transporter (ABCA4) and all-trans-retinol dehydrogenase (RDH). All-trans-retinal induces Bax activation via DNA damage to mediate retinal cell apoptosis .
    All-trans-retinal
  • HY-N0364
    Falcarindiol
    1 Publications Verification

    		 Apoptosis Autophagy PPAR Infection Metabolic Disease Inflammation/Immunology Cancer
    Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties . Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Falcarindiol
  • HY-172778
    HNW005

    		NOD-like Receptor (NLR) URAT1 Metabolic Disease Inflammation/Immunology
    HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis .
    HNW005
  • HY-134356
    AICA-riboside, 5′-phosphate

    AICAR-5'-MP

    		 Endogenous Metabolite Others
    AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
    AICA-riboside, 5′-phosphate
  • HY-161501
    3-Fluoro-evodiamine glucose

    		GLUT Topoisomerase Apoptosis Cancer
    3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
    3-Fluoro-evodiamine glucose
  • HY-111191
    ONO-2952
    1 Publications Verification

    		 Adrenergic Receptor Neurological Disease
    ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment .
    ONO-2952
  • HY-117006
    E1231
    1 Publications Verification

    1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one

    		 Sirtuin Cardiovascular Disease
    E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
    E1231
  • HY-123056A
    EAD1 TFA

    		Autophagy Apoptosis Others
    EAD1 TFA is an aluminum-activated malate transporter with activity in regulating corn ear development. EAD1 TFA is preferentially expressed in the xylem of immature ears and localized across the plasma membrane. The EAD1 TFA transports malic acid in the apical part of developing inflorescences, and its deletion results in reduced malic acid content in this part. The overexpression of EAD1 TFA was significantly positively correlated with ear length and the number of kernels per row. EAD1 TFA serves as a potential genetic resource to help improve grain yield in maize .
    EAD1 TFA
  • HY-128574
    D927

    DS11252927

    		 GLUT PI3K Akt Metabolic Disease
    D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes .
    D927
  • HY-103216A
    RWJ52353 hydrochloride

    		Adrenergic Receptor Neurological Disease
    RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
    RWJ52353 hydrochloride
  • HY-173444
    HDAC11-IN-3

    		HDAC Transferrin Receptor Apoptosis Ferroptosis Cancer
    HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC50: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC50: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research .
    HDAC11-IN-3

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